ml-137

ML-137 is a positive allosteric modulator (PAM) of M1 muscarinic acetylcholine receptors (mAChRs). ML-137 potentiates ACh-induced activation of the M1 muscarinic receptor (EC50 = 0.83 µM).

EGFR-IN-137 (Compound 4c) acts as an inhibitor of aromatase and EGFR, with IC50 values of 1.67 μg mL and 0.08 μg mL, respectively. It hinders the proliferation of cancer cells MCF-7 and MDA-MB-231, with IC50 values of 1.62 µM and 4.14 µM. Additionally, EGFR-IN-137 induces cell cycle arrest at the G0 G1 phase in MDA-MB-231 cells and triggers apoptosis through a caspase-dependent pathway.

Emestrin, a mycotoxin originally isolated from *E. striata*, exhibits antimicrobial, immunomodulatory, and cytotoxic activities. It is effective against fungi *C. albicans* and *C. neoformans*, and bacteria *E. coli*, *S. aureus*, and methicillin-resistant *S. aureus* (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg ml, respectively). Emestrin acts as a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes). At 0.1 μg ml, it induces apoptosis in HL-60 cells and causes necrosis in heart, thymus, and liver tissues in mice at doses of 18-30 mg kg.